Evidence for the presence of a septide-sensitive tachykinin receptor in the circular muscle of the guinea-pig ileum

Eur J Pharmacol. 1993 Apr 28;235(2-3):309-11. doi: 10.1016/0014-2999(93)90152-8.

Abstract

The selective tachykinin NK1 receptor agonists, septide ([Glp6,Pro9]substance P-(6-11)) and [Sar9]substance P sulfone, both produced concentration-dependent contraction of the circular muscle of the guinea-pig ileum (EC50 values 36 and 84 pM, respectively). The potent and selective NK1 receptor antagonist (+/-)-CP 96,345 antagonized the response to septide with significantly higher affinity than it did the response to [Sar9]substance P sulfone (pA2 values 9.24 and 8.17, respectively) without modifying the response to the selective NK2 receptor agonist, [beta-Ala8]neurokinin A-(4-10). These findings indicate that the septide-sensitive receptor in the circular muscle of the guinea-pig ileum is recognized with high affinity by the NK1 receptor selective antagonist (+/-)-CP 96,345.

MeSH terms

  • Animals
  • Biphenyl Compounds / pharmacology
  • Dose-Response Relationship, Drug
  • Guinea Pigs
  • Ileum / drug effects*
  • In Vitro Techniques
  • Male
  • Muscle Contraction / drug effects
  • Muscles / drug effects*
  • Neurokinin A / pharmacology
  • Peptide Fragments / pharmacology*
  • Pyrrolidonecarboxylic Acid / analogs & derivatives
  • Receptors, Neurokinin-2
  • Receptors, Neurotransmitter / drug effects*
  • Receptors, Tachykinin
  • Substance P / analogs & derivatives*
  • Substance P / pharmacology
  • Tachykinins / pharmacology

Substances

  • Biphenyl Compounds
  • Peptide Fragments
  • Receptors, Neurokinin-2
  • Receptors, Neurotransmitter
  • Receptors, Tachykinin
  • Tachykinins
  • Substance P
  • septide
  • Neurokinin A
  • neurokinin A(4-10)
  • Pyrrolidonecarboxylic Acid
  • CP 96345